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2965
observed by autoradiography were consistent with the data ob-
tained by the regional brain tissue dissection method (Fig. 2).
In conclusion, we report a series of novel N-fluoropyridyl-con-
taining tropane derivatives with binding affinity and selectivity
to DAT over SERT and NET. Within this series, compound 6d
showed the highest binding affinity to DAT (Ki = 4.1 nM) and selec-
tivity over SERT and NET. Radiolabeling of [18F]6d was successful.
Regional brain distribution and ex vivo autoradiography studies
of [18F]6d demonstrated high specific binding in the striatum.
These results suggest that further exploration of its derivatives as
new imaging agents for the DAT in the brain is warranted.
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This work was supported by grant from the National 973
Program (2006CB500705 and 2011CB504100) from Ministry of
Science and Technology and the National 863 Program
(2006AA02A408), China.
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